CN113454069A - 1,2,4-三嗪-3,5-二酮类化合物及其制备方法和应用 - Google Patents

1,2,4-三嗪-3,5-二酮类化合物及其制备方法和应用 Download PDF

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Publication number
CN113454069A
CN113454069A CN202080005958.3A CN202080005958A CN113454069A CN 113454069 A CN113454069 A CN 113454069A CN 202080005958 A CN202080005958 A CN 202080005958A CN 113454069 A CN113454069 A CN 113454069A
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Prior art keywords
substituted
unsubstituted
triazine
dichloro
group
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CN202080005958.3A
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English (en)
Inventor
吕贺军
王朋
梁辉
郭飞
叶文武
任利锋
刘俊
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Shanghai Kunheng Medical Technology Co ltd
KPC Pharmaceuticals Inc
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Shanghai Kunheng Medical Technology Co ltd
KPC Pharmaceuticals Inc
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Publication of CN113454069A publication Critical patent/CN113454069A/zh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

本发明提供了一种1,2,4‑三嗪‑3,5‑二酮类化合物及其制备方法和应用,本发明提供的具有式(I)所示结构的,2,4‑三嗪‑3,5‑二酮类化合物对THRβ具有选择性激动作用,其活性、选择性和代谢稳定性相对于已公开化合物存在显著优势,能够作为甲状腺激素受体相关疾病的治疗和/或预防药物来发挥作用,甲状腺激素受体相关疾病包括但不限于肥胖、糖尿病、高胆固醇血症、高脂血症、高甘油三酯血症、肝脏脂肪病变、非酒精性脂肪肝、非酒精性脂肪性肝炎、家族性高胆固醇血症、血脂异常、动脉粥样硬化症、甲状腺功能减退症、甲状腺癌。

Description

PCT国内申请,说明书已公开。

Claims (10)

  1. PCT国内申请,权利要求书已公开。
CN202080005958.3A 2019-11-26 2020-11-25 1,2,4-三嗪-3,5-二酮类化合物及其制备方法和应用 Pending CN113454069A (zh)

Applications Claiming Priority (3)

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CN2019111774827 2019-11-26
CN201911177482 2019-11-26
PCT/CN2020/131367 WO2021104288A1 (zh) 2019-11-26 2020-11-25 1,2,4-三嗪-3,5-二酮类化合物及其制备方法和应用

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CN113454069A true CN113454069A (zh) 2021-09-28

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US (1) US20230089582A1 (zh)
EP (1) EP4083024A4 (zh)
JP (1) JP2023503154A (zh)
CN (1) CN113454069A (zh)
CA (1) CA3158379A1 (zh)
TW (1) TWI763147B (zh)
WO (1) WO2021104288A1 (zh)

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WO2022184177A1 (zh) * 2021-03-04 2022-09-09 甫康(上海)健康科技有限责任公司 一种芳香化合物、其制备方法及其应用
CN115073429A (zh) * 2021-03-15 2022-09-20 昆药集团股份有限公司 一种1,2,4-三嗪-3,5-二酮类化合物的盐型、晶型及其制备方法
CN115583920A (zh) * 2022-08-31 2023-01-10 浙江大学 一种四嗪类化合物及其制备方法和应用

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TW202342457A (zh) * 2022-02-07 2023-11-01 大陸商四川海思科製藥有限公司 一種嗒𠯤酮衍生物製備方法及其中間物

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WO2021057791A1 (zh) * 2019-09-24 2021-04-01 广东东阳光药业有限公司 一种作为甲状腺激素Beta受体激动剂的化合物及其用途
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CN105008335A (zh) * 2012-09-17 2015-10-28 马德里加尔制药公司 合成甲状腺激素类似物及其多形体的方法
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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022184177A1 (zh) * 2021-03-04 2022-09-09 甫康(上海)健康科技有限责任公司 一种芳香化合物、其制备方法及其应用
CN115073429A (zh) * 2021-03-15 2022-09-20 昆药集团股份有限公司 一种1,2,4-三嗪-3,5-二酮类化合物的盐型、晶型及其制备方法
CN115583920A (zh) * 2022-08-31 2023-01-10 浙江大学 一种四嗪类化合物及其制备方法和应用
CN115583920B (zh) * 2022-08-31 2024-02-20 浙江大学 一种四嗪类化合物及其制备方法和应用

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CA3158379A1 (en) 2021-06-03
TW202120498A (zh) 2021-06-01
US20230089582A1 (en) 2023-03-23
JP2023503154A (ja) 2023-01-26
EP4083024A1 (en) 2022-11-02
TWI763147B (zh) 2022-05-01
WO2021104288A1 (zh) 2021-06-03
EP4083024A4 (en) 2023-11-01

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